Muscarinic receptor agonists

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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546256, A61K 314439, C07D41714

Patent

active

060967676

ABSTRACT:
A compound of Formula (I): ##STR1## wherein R is a linkage independently selected from (CH.sub.2).sub.12 or (CH.sub.2).sub.4 O.sub.3 ; and acid addition salts, solvates and hydrates thereof. The compounds have unusually high affinity for muscarinic receptors, and exhibit agonist activity useful in the treatment of neurological and other disorders, in which stimulating cholinergic activity is desirable.

REFERENCES:
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Philip G. Dunbar, Graham J. Durant, Zheng Fang, Yahaya F. Abuh, Afif A. El-Assadi, Dan O. Ngur, Sumudra Periyasamy, Wayne P. Hoss and William S. Messer, Jr., Design, Synthesis, and Neurochemical Evaluation of 5-(3-Alkyl-1,2,4-oxadiazol-5-yl)-1,4,5,6-tetrahydropyrimidines as M.sub.1 Muscarinic Receptor Agonists, J. Med. Chem. (1993), 36, pp. 842-847.
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Per Sauerberg, Lone Jeppesen, Preben H. Olesen, Th.o slashed.ger Rasmussen, Michael D.B. Swedberg, Malcolm J. Sheardown, Anders Fink-Jensen, Christian Thomsen, Henning Th.o slashed.gersen, Karin Rimvall, John S. Ward, David O. Calligaro, Neil W. DeLapp, Frank P. Bymaster and Harlan E. Shannon, Muscarinic Agonists with Antipsychotic-like Activity: Structure-Activity Relationships of 1,2,5-Thiadiazole Analogues with Functional Dopamine Antagonist Activity, J. Med. Chem. (1998), 41, pp. 4378-4384.
Lone Jeppesen, Preben H. Olesen, Lena Hansen, Malcolm J. Sheardown, Christian Thomsen, Th.o slashed.ger Rasmussen, Anders Fink Jensen, Michael S. Christensen, Karin Rimvall, John S. Ward, Celia Whitesitt, David O. Calligaro, Frank P. Bymaster, Neil W. DeLapp, Christian C. Felder, Harlan E. Shannon, and Per Sauerberg, 1,(1,2,5-Thiadiazol-4-yl)-4-azatricyclo[2.2.1.0.sup.2,6 ]heptanes as New Potent Muscarinic M.sub.1 Agonists: Structure-Activity Relationship for 3-Aryl-2-propyn-1-yloxy and 3-Aryl-2-propyn-1-ylthio Derivatives, J. Med. Chem. (1999), 42, pp. 1999-2006.

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